联苯苄唑的兔药代动力学研究及组织残留量测定

Pharmacokinetics of Bifonazole in Rabbits and Quantitative Determination of Concentration in Organs

  • 摘要: 采用 GC/ MS单离子检测的方法测定了联苯苄唑溶液剂和霜剂在家兔皮肤抹药后的血药浓度和在肝、胃、皮肤等组织中的药物浓度 ;并用 3P87软件对血药浓度进行了拟合 ,估算了药物动力学参数。结果表明 ,溶液剂和霜剂的体内过程均符合二室开放模型 ,Tmax 分别为 2 .88h和 5 .84h,Cmax 分别为35 6 .1 8ng/ ml和 1 82 .81 ng/ ml。在组织联苯苄唑含量测定中 ,只有用药局部皮肤有残留 ,而肝、胃和肌肉等组织中没有联苯苄唑残留。

     

    Abstract: The bifonazole's plasma concentration in rabbits after bifonazole solution preparation and cream preparation spread on rabbit skin was determined,using GC/MS-SIM quantitative method,and their pharmacokinetic parameters were calculated with 3p87 software.The results showed that the plasma concentration-time curves of the two preparations in rabbits were fitted to the two-compartment open model.Tmax of solution and cream preparations were 2.84 h and 5.84 h,and Cmax,356.18ng/ml and 182.81ng/ml,respectively.The concentration of bifonazole in drug-spread skin was quantified:4200ng after one day,2500ng after two days,and 1250ng after three days respectively.However,the concentrations of bifonazole in liver,kidney,muscle,muscle beneath skin and skin for control are lower than the determination limit.

     

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